[3H]aldosterone [Ligand Id: 3452] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL273453 (Aldosterone, NSC-73856)
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • Corticosteroid binding globulin in Human [ChEMBL: CHEMBL2421] [UniProtKB: P08185]
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  • Testis-specific androgen-binding protein in Human [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 4.37 pIC50 >42657.95 nM IC50 J. Med. Chem. (2005) 48: 5666-5674 [PMID:16134935]
Corticosteroid binding globulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2421] [UniProtKB: P08185]
ChEMBL Binding affinity to human CBG receptor (corticosteroid-binding globulins) B 6.28 pKi 524.81 nM Ki J. Med. Chem. (2004) 47: 2732-2742 [PMID:15139751]
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
ChEMBL Binding affinity to MR (unknown origin) B 9.3 pKd 0.5 nM Kd J Med Chem (2017) 60: 2629-2650 [PMID:28051871]
ChEMBL Antagonist activity at mineralocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay F 8.03 pIC50 9.27 nM IC50 J. Med. Chem. (2010) 53: 6947-6953 [PMID:20812681]
ChEMBL Agonist activity at GAL4 DNA-binding domain fused MR (unknown origin) ligand binding domain expressed in UAS-bla H cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay B 9.52 pIC50 0.3 nM IC50 Eur J Med Chem (2018) 157: 791-804 [PMID:30144697]
ChEMBL Agonist activity at mineralocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay B 8.42 pEC50 3.8 nM EC50 J. Nat. Prod. (2009) 72: 1944-1948 [PMID:19863083]
ChEMBL Agonist activity at mineralocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay F 9.47 pEC50 0.34 nM EC50 J. Med. Chem. (2010) 53: 6947-6953 [PMID:20812681]
ChEMBL Agonist activity at human MCR expressed in HEK293 cells by luciferase reporter gene assay B 9.74 pEC50 0.18 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 5265-5267 [PMID:25305688]
Mineralocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3507] [GtoPdb: 626] [UniProtKB: P22199]
GtoPdb - - 9.52 pKd 0.3 nM Kd Am. J. Physiol. (1984) 246: F227-33 [PMID:6320679];
Mol. Cell. Endocrinol. (2005) 243: 35-42 [PMID:16188378]
ChEMBL Displacement of [3H]aldosterone from Sprague-Dawley rat MR by liquid scintillation counting B 7.37 pIC50 43 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1744-1747 [PMID:21349712]
ChEMBL Displacement of [3H]Aldo from mineralocorticoid receptor in Sprague-Dawley rat kidney after 2 hrs by liquid scintillation counting B 7.37 pIC50 43 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6310-6313 [PMID:21944856]
Testis-specific androgen-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3305] [UniProtKB: P04278]
ChEMBL Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin B 5.32 pKd 4786.3 nM Kd J. Med. Chem. (2008) 51: 2047-2056 [PMID:18330978]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]